Elbasvir-MK-8742-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEElbasvirCat.No.:HY-15789CASNo.:1370468-36-2Synonyms:MK-8742分⼦式:C₄₉H₅₅N₉O₇分⼦量:882.02作⽤靶点:HCV作⽤通路:Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥50mg/mL(56.69mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.1338mL5.6688mL11.3376mL5mM0.2268mL1.1338mL2.2675mL10mM0.1134mL0.5669mL1.1338mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(2.83mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(2.83mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Elbasvir(MK-8742)丙型肝炎病毒⾮结构蛋⽩5A(HCVNS5A)抑制剂，对因型1a，1b和2a的EC50分别为4，3和3nM。IC50&TargetEC50:4nM(HCV1a),3nM(HCV1b),3nM(HCV2a)[1]体外研究Elbasvirshowspotentactivityagainstgenotype1aand1breplicons,withEC90of0.006nMforboththewild-type1a_H77and1b_con1replicons.Elbasvirinhibitsgenotype3repliconswithEC90of0.12nM.Elbasvir(0.06nM,0.6nM,and6nM)demonstratesdose-dependentsuppressionofresistantgenotype1areplicons,illustratedbythereductionsincolonycountsathigherdoses[1].ElbasvirishighlypotentagainstHCVrepliconsbearingNS5AsequencesfromGT1a,-1b,-2a(31L),-3a,-4a,-5a,and-6,withEC50sinthelow-picomolarrange[2].户使⽤本产品发表的科研⽂献•AdvSci(Weinh).2022Oct18;e2203088.•Hepatology.2019May;69(5):1861-1872.•JGastroenterol.2019May;54(5):449-458.•Viruses.2018Aug28;10(9).pii:E462.•Pharmaceuticals.2022Feb18;15(2):242.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LiuR,etal.Susceptibilitiesofgenotype1a,1b,and3hepatitisCvirusvariantstotheNS5AinhibitorElbasvir.AntimicrobAgentsChemother.2015Nov;59(11):6922-6929.[2].LahserFC,etal.TheCombinationofGrazoprevir,aHepatitisCVirus(HCV)NS3/4AProteaseInhibitor,andElbasvir,anHCVNS5AInhibitor,DemonstratesaHighGeneticBarriertoResistanceinHCVGenotype1aReplicons.AntimicrobAgentsChemother.2016AMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F